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Assay Detail

CHEMBL816539

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of Tripeptidyl-peptidase II purified from a rat liver post-lysosomal fraction.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Tripeptidyl-peptidase 2 (CHEMBL4675)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Tripeptidyl-peptidase II (TPP II) inhibitory activity of (S)-2,3-dihydro-2-(1H-imidazol-2-yl)-1H-indoles, a systematic SAR evaluation. Part 2.
Breslin HJ, Miskowski TA, Kukla MJ, De Winter HL, Somers MV, Roevens PW, Kavash RW.
Bioorg Med Chem Lett (2003) 13 : 4467 -4471
PubMed 14643348 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 7.44 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL341545 1 8.40
CHEMBL141228 1 8.40
CHEMBL344682 1 8.30
CHEMBL140029 1 8.22
CHEMBL345086 1 7.96
CHEMBL140875 1 7.70
CHEMBL337314 1 7.64
CHEMBL337540 1 7.44
CHEMBL138968 1 7.34
CHEMBL138058 1 7.16
CHEMBL344851 1 6.71
CHEMBL138313 1 5.85
CHEMBL138518 1 5.64
CHEMBL137926 1 -
CHEMBL341589 1 -
CHEMBL138051 1 -
CHEMBL443220 1 -
CHEMBL139137 1 -
CHEMBL138160 1 -
CHEMBL343528 1 -
CHEMBL436012 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL341545 IC50 = 4.0 nM 8.40
CHEMBL141228 IC50 = 4.0 nM 8.40
CHEMBL344682 IC50 = 5.0 nM 8.30
CHEMBL140029 IC50 = 6.0 nM 8.22
CHEMBL345086 IC50 = 11.0 nM 7.96
CHEMBL140875 IC50 = 20.0 nM 7.70
CHEMBL337314 IC50 = 23.0 nM 7.64
CHEMBL337540 IC50 = 36.0 nM 7.44
CHEMBL138968 IC50 = 46.0 nM 7.34
CHEMBL138058 IC50 = 70.0 nM 7.16
CHEMBL344851 IC50 = 194.0 nM 6.71
CHEMBL138313 IC50 = 1400.0 nM 5.85
CHEMBL138518 IC50 = 2300.0 nM 5.64
CHEMBL137926 IC50 > 10000.0 nM -
CHEMBL341589 IC50 > 10000.0 nM -
CHEMBL138051 IC50 > 10000.0 nM -
CHEMBL443220 IC50 > 10000.0 nM -
CHEMBL139137 IC50 > 10000.0 nM -
CHEMBL138160 IC50 > 10000.0 nM -
CHEMBL343528 IC50 > 10000.0 nM -
CHEMBL436012 IC50 > 10000.0 nM -